Endodontic pharmacology /prosthodontic courses

ENDODONTICENDODONTIC
PHARMACOLOGYPHARMACOLOGY
INDIAN DENTAL ACADEMY
Leader in continuing Dental
Education
www.indiandentalacademy.comwww.indiandentalacademy.com

CONTENTSCONTENTS
IntroductionIntroduction
Antibiotic therapy in management of infectionsAntibiotic therapy in management of infections
a- definitiona- definition
b- principles of therapyb- principles of therapy
c- principles of antibiotic selectionc- principles of antibiotic selection
d- principles of antibiotic administrationd- principles of antibiotic administration
ClassificationClassification
a- based on chemical sructurea- based on chemical sructure
b- type of organisms on which it actsb- type of organisms on which it acts
c- bacteristatic/ bacteriocidalc- bacteristatic/ bacteriocidal
d- chemotherapeutic spectrad- chemotherapeutic spectra
Mechanism of actionMechanism of action

 Antibiotics commonly used in endodonticsAntibiotics commonly used in endodontics
1.1. PenicillinsPenicillins
2.2. CephalosporinsCephalosporins
3.3. QuinolonesQuinolones
4.4. TetracyclinesTetracyclines
5.5. MacrolidesMacrolides
6.6. Antifungal agentsAntifungal agents
7.7. Antiviral agentsAntiviral agents
 Antibiotic Prophylaxis for Heart and ArtificialAntibiotic Prophylaxis for Heart and Artificial
Joint PatientsJoint Patients
 Analgesics used in endodonticsAnalgesics used in endodontics
1.1. IntroductionIntroduction
2.2. DefinitionDefinition
3.3. PropertiesProperties

Classification of PainClassification of Pain
Pain PathwaysPain Pathways
Management of painManagement of pain
1.1. OpioidOpioid
2.2. Non-opioidNon-opioid
a- classificationa- classification
b- mechanism of actionb- mechanism of action
Anti-anxiety DrugsAnti-anxiety Drugs
Other drugsOther drugs
Root-canal IrrigantsRoot-canal Irrigants
Intra-canal medicamentsIntra-canal medicaments
Mummyfing agentsMummyfing agents
StypticsStyptics
ReferencesReferences

PHARMACOLOGY:PHARMACOLOGY:
science of drugs and their interaction with thescience of drugs and their interaction with the
living systemsliving systems
DRUG (Def) (WHO) - a drug is defined as anyDRUG (Def) (WHO) - a drug is defined as any
substance or product that is used or intended to be usedsubstance or product that is used or intended to be used
to modify or explore physiological systems orto modify or explore physiological systems or
pathological states for the benefit of the recipientpathological states for the benefit of the recipient
Drugs are important in Endodontics to fight againstDrugs are important in Endodontics to fight against
1. infections1. infections
2. pain2. pain
3.anxiety3.anxiety

ANTIBIOTIC THERAPYANTIBIOTIC THERAPY
IN MANAGEMENT OF INFECTIONSIN MANAGEMENT OF INFECTIONS

Bacterial pathways to the pulp:Bacterial pathways to the pulp:
1. caries1. caries
2. periodontal disease2. periodontal disease
3. fractures3. fractures
4. dentinal tubules not covered4. dentinal tubules not covered
5. Anachoresis5. Anachoresis
Pulpal invasion begins with a mixedPulpal invasion begins with a mixed
infection of aerobes and anaerobesinfection of aerobes and anaerobes
As oxygen is depleted obligate anaerobicAs oxygen is depleted obligate anaerobic
bacteria and facultative bacteriabacteria and facultative bacteria
predominate.predominate.

Primary goal of endodontic treatment is toPrimary goal of endodontic treatment is to
eliminate a hospitable place foreliminate a hospitable place for
microorganisms to grow.microorganisms to grow.
1. debridement of canal should be1. debridement of canal should be
as thorough as possibleas thorough as possible
2.total obturation of the space to2.total obturation of the space to
close off the path for oral bacteria to reachclose off the path for oral bacteria to reach
beyond the apexbeyond the apex
3. use of sterile technique to avoid3. use of sterile technique to avoid
introducing any new microbesintroducing any new microbes

But in situations where infections exist beyond the rootBut in situations where infections exist beyond the root
canal it is advisable to use systemic antibiotics.canal it is advisable to use systemic antibiotics.
Chemotherapy- is defined as the use of synthetic,Chemotherapy- is defined as the use of synthetic,
semisynthetic, and naturally occuring chemicals thatsemisynthetic, and naturally occuring chemicals that
selectively inhibit specific organisms causing disease.selectively inhibit specific organisms causing disease.
ANTIBIOTICSANTIBIOTICS
are antibacterial agents which are used to killare antibacterial agents which are used to kill
bacteria without damage to the host.bacteria without damage to the host.
1. more appropriate term is antimicrobial agents1. more appropriate term is antimicrobial agents
2.they are obtained naturally as well as synthetically2.they are obtained naturally as well as synthetically

DefinitionsDefinitions
Antimicrobials – are substances that kill orAntimicrobials – are substances that kill or
suppress the growth or multiplication ofsuppress the growth or multiplication of
microorganisms, either bacteria, viruses,microorganisms, either bacteria, viruses,
fungi, or parasites.fungi, or parasites.
Antibiotics – substances produced byAntibiotics – substances produced by
microorganisms or by synthetic chemicalmicroorganisms or by synthetic chemical
methods that have the capability tomethods that have the capability to
produce an antibacterial action.produce an antibacterial action.

Principles of therapyPrinciples of therapy
Presence of infectionPresence of infection
State of host defensesState of host defenses
Surgical drainage and incisionSurgical drainage and incision

Presence of infection:Presence of infection:
– Local Signs of infection: pain, swelling,Local Signs of infection: pain, swelling,
erythema, pus formation, and limitation oferythema, pus formation, and limitation of
motion should be noted.motion should be noted.
– Systemic signs : fever, lymphadenopathy,Systemic signs : fever, lymphadenopathy,
malaise, toxic appearance, and leucocytosis.malaise, toxic appearance, and leucocytosis.
Non-infectious conditions:Non-infectious conditions:
– Removal of third molar, major surgeries of theRemoval of third molar, major surgeries of the
maxillofacial region – lead to swelling andmaxillofacial region – lead to swelling and
pain.pain.
In the above conditions proper diagnosisIn the above conditions proper diagnosis
plays a very important roleplays a very important role

State of host defenses:State of host defenses:
– Host defense mechanisms are the mostHost defense mechanisms are the most
important factor in the final outcome ofimportant factor in the final outcome of
bacterial insult.bacterial insult.
– It is provided by the white blood cells andIt is provided by the white blood cells and
antibodies produced.antibodies produced.
– It is necessary to evaluate the state of hostIt is necessary to evaluate the state of host
defense mechanism.defense mechanism.
– Infections are ultimately cured by host thanInfections are ultimately cured by host than
antibiotics is critical.antibiotics is critical.
– Antibiotics help in conditions where the hostAntibiotics help in conditions where the host
has been overwhelmed by bacteria.has been overwhelmed by bacteria.

Surgical drainage and incision :Surgical drainage and incision :
– It is an established principle of treatment ofIt is an established principle of treatment of
deep tissue infections.deep tissue infections.
– The objective is to drain pus from tissueThe objective is to drain pus from tissue
spaces and to insert drains so that no pusspaces and to insert drains so that no pus
accumulates in these spaces.accumulates in these spaces.
– In odontogenic infections – removal of tooth,In odontogenic infections – removal of tooth,
opening of the pulp chamber.opening of the pulp chamber.
– Surgical incision – in cellulitis without pusSurgical incision – in cellulitis without pus
formation.formation.

Principles of antibiotic selectionPrinciples of antibiotic selection
– Identification of the causative organism.Identification of the causative organism.
– Determination of antibiotic sensitivity.Determination of antibiotic sensitivity.
– Use a specific, narrow spectrum antibioticUse a specific, narrow spectrum antibiotic
– Use the least toxic drug.Use the least toxic drug.
– Bacteriostatic vs Bactericidal.Bacteriostatic vs Bactericidal.
– Use of antibiotic with a proven history ofUse of antibiotic with a proven history of
success.success.
– Cost of the antibiotic.Cost of the antibiotic.
– Encourage patient compliance.Encourage patient compliance.

Identification of the causativeIdentification of the causative
organism:organism:
Can be done by isolating the organism from pus,Can be done by isolating the organism from pus,
blood, or tissue.blood, or tissue.
Antibiotic therapy is then either initial orAntibiotic therapy is then either initial or
definitive.definitive.
Initial empirical therapy may be started if the followingInitial empirical therapy may be started if the following
criteria are met:criteria are met:
– Site and features of infection are well defined.Site and features of infection are well defined.
– The circumstances leading to infection are known.The circumstances leading to infection are known.
– the organism/s causing the disease are known.the organism/s causing the disease are known.

The typical odontogenic infection – aerobic andThe typical odontogenic infection – aerobic and
anaerobic bacteria.anaerobic bacteria.
– Approx 70% - mixed floraApprox 70% - mixed flora
– 25% - pure anaerobic25% - pure anaerobic
– 5% -aerobic.5% -aerobic.
It has been reported that the bacteria found inIt has been reported that the bacteria found in
cellulitis type of infections – aerobic bacteria.cellulitis type of infections – aerobic bacteria.
Chronic non-advancing abscess – anaerobicChronic non-advancing abscess – anaerobic
bacteria.bacteria.
As the infection becomes severe- mixed floraAs the infection becomes severe- mixed flora

Odontogenic infectionsOdontogenic infections
AerobicAerobic AnaerobicAnaerobic
Gram negative
rods
50%
Bacteriodes
Fusobacterium
Gram positive
cocci-30%
Streptococci
peptostreptococci
Gram positive
S.Milleri
S. Salivarius
S.Sanguis
S. mutans.

BacteroidsBacteroids
Porphyromonas ProvetellaPorphyromonas Provetella
P .gingivalis
P .denticola
P . asaccharolytics
More common .
P .melanogenica
P .denticola
P. Intermedia
P .buccae

Principles of antibioticPrinciples of antibiotic
administrationadministration
Proper doseProper dose
Proper time intervalProper time interval
Proper route of administrationProper route of administration
Consistency in route of administrationConsistency in route of administration
Combination of antibiotic therapyCombination of antibiotic therapy

Proper doseProper dose
Minimum inhibitory concentration (MIC) ofMinimum inhibitory concentration (MIC) of
the drug should be known.the drug should be known.
For therapeutic purposes the peakFor therapeutic purposes the peak
concentration of the drug at the site ofconcentration of the drug at the site of
infection is 3-4times MIC.infection is 3-4times MIC.

Therapeutic levels greater than 3-4timesTherapeutic levels greater than 3-4times
the MIC do not improve the results. Leadsthe MIC do not improve the results. Leads
to toxicity and is wasteful.to toxicity and is wasteful.
Increased doses are justified when the siteIncreased doses are justified when the site
is isolated from the blood supply, likeis isolated from the blood supply, like
abcess or nonvital tissue.abcess or nonvital tissue.
Sufficient antibiotic must be given to reachSufficient antibiotic must be given to reach
the therapeutic levels.the therapeutic levels.
Sub therapeutic doses may mask theSub therapeutic doses may mask the
infection and suppress the clinicalinfection and suppress the clinical
symptoms .symptoms .
May cause recurrence of infection.May cause recurrence of infection.

Proper time interval:Proper time interval:
Knowledge of the pharmacokinetics of theKnowledge of the pharmacokinetics of the
drug should be known.drug should be known.
The usual dosage interval for therapeuticThe usual dosage interval for therapeutic
use of antibiotics is – 4times the tuse of antibiotics is – 4times the t½½
(plasma half life)(plasma half life)
Patient should be evaluated for h/o renalPatient should be evaluated for h/o renal
diseases. They have reduced renaldiseases. They have reduced renal
clearance and may require longer timeclearance and may require longer time
interval between doses.interval between doses.

Proper route of administrationProper route of administration
Serious, established infection – parenteralSerious, established infection – parenteral
route.route.
After initial response is achieved, the routeAfter initial response is achieved, the route
of administration should not be changedof administration should not be changed
immediately.immediately.
The infection may recur because theThe infection may recur because the
blood levels of the drug may be reduced.blood levels of the drug may be reduced.
Bacteria are not eradicated until theBacteria are not eradicated until the
antibiotic has been given for 5 or 6 days.antibiotic has been given for 5 or 6 days.

Combination of antibioticsCombination of antibiotics
Combination should be avoided when notCombination should be avoided when not
indicated.indicated.
The result of combination:The result of combination:
– Broad spectrum exposure that leads to depression ofBroad spectrum exposure that leads to depression of
the normal host flora and increased opportunity forthe normal host flora and increased opportunity for
resistant bacteria to emerge.resistant bacteria to emerge.
Indications :Indications :
– Necessity to increase the antibacterial spectrum, inNecessity to increase the antibacterial spectrum, in
patients with life threatening conditions.patients with life threatening conditions.
– When increased bactericidal effect against a specificWhen increased bactericidal effect against a specific
organism is required.organism is required.
– Prevention of emergence of resistant bacteriaPrevention of emergence of resistant bacteria

Patient monitoringPatient monitoring
Response to treatment:Response to treatment:
– Patients rarely have a noticeable response –Patients rarely have a noticeable response –
24-48hrs.24-48hrs.
– The response begins the second day.The response begins the second day.
– Eradication of infection is generally achievedEradication of infection is generally achieved
by the third day.by the third day.
– Usually 7 - day course is indicated.Usually 7 - day course is indicated.
– If no improvement is seen on 3If no improvement is seen on 3rdrd
or 4or 4thth
day- theday- the
patient should be carefully re-evaluated.patient should be carefully re-evaluated.
– The antibiotic has to be reevaluated.The antibiotic has to be reevaluated.

CLASSIFICATION OF ANTIBIOTICSCLASSIFICATION OF ANTIBIOTICS
Based on chemical structureBased on chemical structure
Type of organisms on which it actsType of organisms on which it acts
Bacteriostatic/BacteriocidalBacteriostatic/Bacteriocidal
Chemotherapeutic spectraChemotherapeutic spectra

Classification of antimicrobialsClassification of antimicrobials
Chemical structureChemical structure
Sulfonamides and related drugsSulfonamides and related drugs
– Sulfadiazine and othersSulfadiazine and others
– Sulfones – Dapsone (DDS), Paraaminosalicylic acid (PAS).Sulfones – Dapsone (DDS), Paraaminosalicylic acid (PAS).
DiaminopyrimidinesDiaminopyrimidines
– TrimethoprimTrimethoprim
– PyrimethaminePyrimethamine
QuinolonesQuinolones
– Nalidixic acidNalidixic acid
– NorfloxacinNorfloxacin
– Ciprofloxacin etcCiprofloxacin etc

ββ-lactam antibiotics-lactam antibiotics
– PenicillinsPenicillins
– CephalosporinsCephalosporins
– MonobactamsMonobactams
– CarbapenemsCarbapenems
TetracyclinesTetracyclines
– OxytetracyclineOxytetracycline
– Doxycycline etcDoxycycline etc
Nitrobenzene derivativeNitrobenzene derivative
– ChloramphenicolChloramphenicol

AminoglycosidesAminoglycosides
– StreptomycinStreptomycin
– GentamicinGentamicin
– Neomycin etcNeomycin etc
Macrolide antibioticsMacrolide antibiotics
– ErythromycinErythromycin
– RoxithromycinRoxithromycin
– Azithromycin etcAzithromycin etc
Polypeptide antibioticsPolypeptide antibiotics
– Polymyxin-BPolymyxin-B
– ColistinColistin
– BacitracinBacitracin

Type of organisms against which primarily activeType of organisms against which primarily active
AntibacterialAntibacterial
– PenicillinsPenicillins
– AminoglycosidesAminoglycosides
– Erythromycin etcErythromycin etc
AntifungalAntifungal
– GriseofulvinGriseofulvin
– Amphotericin BAmphotericin B
– KetoconazoleKetoconazole
AntiviralAntiviral
– IdoxuridineIdoxuridine
– AcyclovirAcyclovir
– AmantadineAmantadine
– Zidovudine etcZidovudine etc

AntiprotozoalAntiprotozoal
– ChloroquineChloroquine
– PyrimethaminePyrimethamine
– MetronidazoleMetronidazole
– Diloxanide etcDiloxanide etc
AnthelminticAnthelmintic
– MebendazoleMebendazole
– PyrantelPyrantel
– NiclosamideNiclosamide
– Diethyl carbamazine etcDiethyl carbamazine etc

BactericidalBactericidal- the ability to kill the bacteria- the ability to kill the bacteria
Bacteriostatic-Bacteriostatic- the ability to inhibit or retardthe ability to inhibit or retard
the growth of bacteriathe growth of bacteria
Bacteriostatic v/s BactericidalBacteriostatic v/s Bactericidal
ChloramphenicolChloramphenicol
ClindamycinClindamycin
erythromycinerythromycin
SulfonamidesSulfonamides
TetracyclineTetracycline
trimethoprimtrimethoprim
Aminoglycosides
Bacitracin
Cephalosporins
Metronidiazole
vancomycin
Penicillins
ciprofloxacin
streptomycin
cotrimoxazole

Chemotherapeutic SpectraChemotherapeutic Spectra
Narrow spectrumNarrow spectrum
Effective against only a few microorganisms with aEffective against only a few microorganisms with a
very specific metabolic pathway or enzyme.very specific metabolic pathway or enzyme.
– Penicillin G, streptomycin, erythromycin.Penicillin G, streptomycin, erythromycin.
Broad spectrumBroad spectrum
Useful in treating a wide variety of infectionsUseful in treating a wide variety of infections
– Ex: tetracycline, chloramphenical, cephalosporinsEx: tetracycline, chloramphenical, cephalosporins

Mechanism of actionMechanism of action

Antibiotics commonly used in EndodonticsAntibiotics commonly used in Endodontics
PenicillinsPenicillins
CephalosporinsCephalosporins
QuinolonesQuinolones
TetracyclinesTetracyclines
MacrolidesMacrolides
Antifungal agentsAntifungal agents
Anti-viral agentsAnti-viral agents

PENICILLINSPENICILLINS

PenicillinPenicillin
First antibiotic toFirst antibiotic to
be used clinicallybe used clinically
in 1941.in 1941.
Originally obtainedOriginally obtained
from the fungus –from the fungus –
P.notatum.P.notatum.
Present source isPresent source is
P.chrysogenum.P.chrysogenum.

These drugs act on the bacterial cellThese drugs act on the bacterial cell
wall by:wall by:
– Interfere with synthesis of peptidoglycanInterfere with synthesis of peptidoglycan
layer in cell walllayer in cell wall
– bind to and inhibit activity of enzymesbind to and inhibit activity of enzymes
transpeptidases, so that cross-linking doestranspeptidases, so that cross-linking does
not take placenot take place
These enzymes and related proteins-“penicillin-These enzymes and related proteins-“penicillin-
binding proteins”binding proteins”
– When bacteria divide in the presence ofWhen bacteria divide in the presence of ββ--
lactam antibiotics- cell wall deficient formslactam antibiotics- cell wall deficient forms
are produced. The interior of the bacteriaare produced. The interior of the bacteria
is hyperosmotic,is hyperosmotic, eventually cause cell lysiseventually cause cell lysis

BENZYL PENICILLIN (PENCILLIN G)BENZYL PENICILLIN (PENCILLIN G)
– PnG is a narrow spectrum antibiotic; activity is limitedPnG is a narrow spectrum antibiotic; activity is limited
primarily to gram positive bacteriaprimarily to gram positive bacteria
Antibacterial activityAntibacterial activity
– Most potent AMA, inhibits the growth of susceptibleMost potent AMA, inhibits the growth of susceptible
organism.organism.
– Mainly gram +ve, gram –ve cocci and some gram +veMainly gram +ve, gram –ve cocci and some gram +ve
bacilli with exception of enterococci.bacilli with exception of enterococci.
– Cocci – Highly sensitive – Streptococci,Cocci – Highly sensitive – Streptococci,
Pneumococci, Staph. aureus, N. gonorrhoeae, N.Pneumococci, Staph. aureus, N. gonorrhoeae, N.
meningitismeningitis
– Bacilli – B. anthracis, Corynebacterium diphtheriae,Bacilli – B. anthracis, Corynebacterium diphtheriae,
clostridium tetany and spirochetesclostridium tetany and spirochetes
– Actinomyces israelii is moderately sensitiveActinomyces israelii is moderately sensitive

SEMI SYNTHETIC PENICILLINSSEMI SYNTHETIC PENICILLINS
The major drawbacks of benzyl penicillin are :The major drawbacks of benzyl penicillin are :
– Inactivation by the gastric hydrochloric acidInactivation by the gastric hydrochloric acid
– Short duration of actionShort duration of action
– Poor penetration into CSFPoor penetration into CSF
– Activity mainly against gram +ve organismActivity mainly against gram +ve organism
– Possibility of anaphylaxisPossibility of anaphylaxis
Attempts therefore have been made to synthesizeAttempts therefore have been made to synthesize
penicillin free from such drawbacks.penicillin free from such drawbacks.
P.chrysogenum produces natural penicillins whichP.chrysogenum produces natural penicillins which
produce the 6 amino- penicillanic acid (6-APA) nucleus.produce the 6 amino- penicillanic acid (6-APA) nucleus.
The attachment of side chains are inhibited and insteadThe attachment of side chains are inhibited and instead
various organic radicals were substituted.various organic radicals were substituted.
Thus a variety of semi synthetic drugs are producedThus a variety of semi synthetic drugs are produced..

CLASSIFICATIONCLASSIFICATION
Acid resistant alternative to penicillin GAcid resistant alternative to penicillin G
(Phenoxy methyl penicillin)(Phenoxy methyl penicillin)
Penicillinase resistant penicillins.Penicillinase resistant penicillins.
(Methicillin,Cloxacillin)(Methicillin,Cloxacillin)
Extended spectrum penicillins(ampicillin,Extended spectrum penicillins(ampicillin,
amoxicillin)amoxicillin)

Acid resistant pencillinsAcid resistant pencillins ::
Potassium phenoxymethyl penicillinPotassium phenoxymethyl penicillin (penicillin V)(penicillin V)
– Similar antibacterial spectrum like benzylpenicillin.Similar antibacterial spectrum like benzylpenicillin.
– More active against resistant staphylococciMore active against resistant staphylococci
– Less inactivated by the gastric acid.Less inactivated by the gastric acid.
– Plasma levels achieved is 2 to 5 times higher thanPlasma levels achieved is 2 to 5 times higher than
benzylpenicillin.benzylpenicillin.
– 50-70% is bound to plasma proteins.50-70% is bound to plasma proteins.
– 25% of drug is eliminated in urine25% of drug is eliminated in urine
– Administered in the dose of 250 –500 mg at 4-8 hoursAdministered in the dose of 250 –500 mg at 4-8 hours
intervals, atleast 30 min before food.intervals, atleast 30 min before food.
– This can be used in less serious infectionsThis can be used in less serious infections
(pneumocci and streptococci)(pneumocci and streptococci)
– Dose –penicillin V 500 mg qid.Dose –penicillin V 500 mg qid.

Extended spectrum penicillinsExtended spectrum penicillins
Amino penicillinsAmino penicillins ::
– AmpicillinAmpicillin ––
– Antibacterial activity is similar to that of PnG but is more effectiveAntibacterial activity is similar to that of PnG but is more effective
than PnG against a variety of gram-ve bacteriathan PnG against a variety of gram-ve bacteria
– Drug is effective against H.influenzae strep.viridans,Drug is effective against H.influenzae strep.viridans,
N.gonorrhea, Salmonella, shigellae, Klebsilla and enterococci.N.gonorrhea, Salmonella, shigellae, Klebsilla and enterococci.
Absorption, fate and excretion :Absorption, fate and excretion :
– Oral absorption is incomplete but adequate.Oral absorption is incomplete but adequate.
– Not degraded by gastric acid.Not degraded by gastric acid.
– Food interferes with absorptionFood interferes with absorption
– Partly excreted in bile and partly by kidneyPartly excreted in bile and partly by kidney

– 0.5-2 gm oral/IM or IV depending on severity0.5-2 gm oral/IM or IV depending on severity
of infection every 6 hoursof infection every 6 hours
– Children : 25-50 mg/kg/dayChildren : 25-50 mg/kg/day
– AMPILIN, ROSCILLIAN, BIOCILIN – 250, 500AMPILIN, ROSCILLIAN, BIOCILIN – 250, 500
mg cap 100mg/ml ped drops, 250 mg/ml drymg cap 100mg/ml ped drops, 250 mg/ml dry
syr, 1 gm/vial injsyr, 1 gm/vial inj

AMOXICILLINAMOXICILLIN ::
– This is a semi-synthetic penicillinThis is a semi-synthetic penicillin
(amino-p-hydroxy-benzylpencillin)(amino-p-hydroxy-benzylpencillin)
– Antibacterial spectrum is similar to AmpicillinAntibacterial spectrum is similar to Ampicillin
but less effective than Ampicillin .but less effective than Ampicillin .
– Oral absorption is better; food does notOral absorption is better; food does not
interfere; higher and more sustained bloodinterfere; higher and more sustained blood
levels are produced.levels are produced.
– It is less protein bond and urinary excretion isIt is less protein bond and urinary excretion is
higher than that of ampicillin.higher than that of ampicillin.
– Incidence of diarrhea is lessIncidence of diarrhea is less

DoseDose ::
– 500 mg tid/qid500 mg tid/qid
– AMOXYLIN, NOVAMOX, SYNAMOX, MOX,AMOXYLIN, NOVAMOX, SYNAMOX, MOX,
AMOXIL 250, 500 mg cap, 125 mg/5ml dryAMOXIL 250, 500 mg cap, 125 mg/5ml dry
syr, 500 mg/vial inj.syr, 500 mg/vial inj.
USES :USES :
TyphoidTyphoid
BronchitisBronchitis
Urinary infectionUrinary infection
SBESBE
GonorrhoeaGonorrhoea

BETA LACTAMASE INHIBITORSBETA LACTAMASE INHIBITORS
CLAVULANIC ACIDCLAVULANIC ACID
– Obtained from STREPTOMYCES CLAVULIGERUSObtained from STREPTOMYCES CLAVULIGERUS
– It has a Beta lactam ring – no antibacterial activityIt has a Beta lactam ring – no antibacterial activity
– Called as Suicide inhibitor –inactivated after bindingCalled as Suicide inhibitor –inactivated after binding
to enzymeto enzyme
– Permeates the outer layers of cell wall of gram-vePermeates the outer layers of cell wall of gram-ve
bacteriabacteria

PharmacokineticsPharmacokinetics ::
– Oral absorption- rapidOral absorption- rapid
– Bioavailability-60%Bioavailability-60%
– Distribution similar that of amoxicillinDistribution similar that of amoxicillin
– Excretion-tubular secretionExcretion-tubular secretion
UsesUses ::
– Staph aureus,H influenza, gonorrhoea and E coliStaph aureus,H influenza, gonorrhoea and E coli
Adverse effectsAdverse effects ::
– Poor g.i. tolerancePoor g.i. tolerance
– HepatotoxicityHepatotoxicity
AUGMENTIN, AMONATE, ENHANCINAUGMENTIN, AMONATE, ENHANCIN
DOSE-Amox 250mg+clavulanic acid 125mg tab,1-2 tab TDS,DOSE-Amox 250mg+clavulanic acid 125mg tab,1-2 tab TDS,
severe infection 4 tabs 6 hourlysevere infection 4 tabs 6 hourly

CEPHALOSPORINSCEPHALOSPORINS

CEPHALOSPORINSCEPHALOSPORINS
Cephalosporium acremonium was the first source.Cephalosporium acremonium was the first source.
They contain 7 amino cephalosporonic acid nucleus.They contain 7 amino cephalosporonic acid nucleus.
Structurally they containStructurally they contain ββ-lactam and dihydro thiazine-lactam and dihydro thiazine
rings.rings.
Mechanism of actionMechanism of action ::
– Act by inhibiting bacterial cell was synthesis and areAct by inhibiting bacterial cell was synthesis and are
bactericidal.bactericidal.
– New derivatives are much more resistant than theNew derivatives are much more resistant than the
older cephalosporinsolder cephalosporins

ClassificationClassification
First generation cephalosporinFirst generation cephalosporin
– Good activity against gram +ve bacteria.Good activity against gram +ve bacteria.
(except enterococci).(except enterococci).
– Most oral cavity anaerobes are sensitive.Most oral cavity anaerobes are sensitive.
– ParentalParental OralOral
– CEPHALOTHINCEPHALOTHIN CEPHALEXINCEPHALEXIN
– CEFAZOLINCEFAZOLIN CEPHRADINECEPHRADINE
CEFADROXILCEFADROXIL

Cephalaxin and CephadroxilCephalaxin and Cephadroxil ::
Useful in treating community acquired, respiratory andUseful in treating community acquired, respiratory and
urinary tract infections and in surgical prophylaxis.urinary tract infections and in surgical prophylaxis.
Not choice for systemic infections.Not choice for systemic infections.
Dose: 250,500mg cap (6-8 hourly)Dose: 250,500mg cap (6-8 hourly)
CefazolinCefazolin ::
For antimicrobial prophylaxis in most surgicalFor antimicrobial prophylaxis in most surgical
procedures.procedures.
Given only IM / IV.Given only IM / IV.
Dose :Dose :
– IM – 0.25g 8 hrly (mild cases) 1g 6 hrly (severe cases).IM – 0.25g 8 hrly (mild cases) 1g 6 hrly (severe cases).
– SPORIDEX, CEPHAXIN, CEPHACILLIN, CEFADROX,SPORIDEX, CEPHAXIN, CEPHACILLIN, CEFADROX,
DROXYLDROXYL

Second generation CephalosporinsSecond generation Cephalosporins
Increased activity against gram –ve organism.Increased activity against gram –ve organism.
More active against anaerobes.More active against anaerobes.
ParenteralParenteral OralOral
CEFUROXIMECEFUROXIME CEFACLORCEFACLOR
CEFOXITINCEFOXITIN CEFUROXIMECEFUROXIME
Cefaclor:Cefaclor:
– is highly effective by oral route.is highly effective by oral route.
– More active against H. influenzae, E coli.More active against H. influenzae, E coli.
Dose :Dose :
– 500mg tid500mg tid
– KEFLOR, CEFTUM, CEFOGEN, FUROXILKEFLOR, CEFTUM, CEFOGEN, FUROXIL

Third generation cephalosporinThird generation cephalosporin
They highly augmented against gram –ve enterobacterThey highly augmented against gram –ve enterobacter
and pseudomonas.and pseudomonas.
Highly resistant toHighly resistant to ββ-lactamase from gram –ve bacteria.-lactamase from gram –ve bacteria.
Less active on gram +ve cocciLess active on gram +ve cocci
– ParenteralParenteral OralOral
– CEFOTAXIMECEFOTAXIME CEFIXIMECEFIXIME
– CEFTIZOXIMECEFTIZOXIME CEFDINIRCEFDINIR
– CEFTRIAXONECEFTRIAXONE CEFTIBUTENCEFTIBUTEN
– CEFTAZIDIMECEFTAZIDIME
– CEFOPERAZONECEFOPERAZONE
Dose :Dose :
– 400mg daily400mg daily
– 200-400mg tab, bid.200-400mg tab, bid.
– CESPAN, CEFOPROX, PROCADAX, CEPODEM, ORFIXCESPAN, CEFOPROX, PROCADAX, CEPODEM, ORFIX

Fourth generation cephalosporinsFourth generation cephalosporins
Developed in 1990 similar to that of 3rd generation.Developed in 1990 similar to that of 3rd generation.
Highly resistant toHighly resistant to ββ-lactamases.-lactamases.
Active against many bacteria resistant to earlier drugs.Active against many bacteria resistant to earlier drugs.
It has high potency and extended spectrum.It has high potency and extended spectrum.
Effective in many serious infections.Effective in many serious infections.
ParenteralParenteral
– CEFEPINE, CEFPIROMECEFEPINE, CEFPIROME
USES :USES :
– Serious and resistant hospital acquired infections.Serious and resistant hospital acquired infections.
– Septicemia,Septicemia,
– Lower respiratory tract infection.Lower respiratory tract infection.
Dose : 1-2g IM / IV 12 hrly.Dose : 1-2g IM / IV 12 hrly.
– CEFROM, CEFORTH – 1g inj.CEFROM, CEFORTH – 1g inj.

UsesUses
Alternatives to penicillins.Alternatives to penicillins.
RTI, UTI and soft tissue infectionRTI, UTI and soft tissue infection
Penicillinase producing staph infection.Penicillinase producing staph infection.
Septicemias.Septicemias.
Surgical prophylaxisSurgical prophylaxis
Meningitis, gonorrheaMeningitis, gonorrhea
TyphoidTyphoid
Mixed aerobic and anaerobic infectionsMixed aerobic and anaerobic infections
Infection by odd organism or hospital infectionsInfection by odd organism or hospital infections
Prophylactic treatment in neutropenic patientsProphylactic treatment in neutropenic patients

QUINOLONESQUINOLONES

QUINOLONESQUINOLONES
Entirely synthetic antimicrobials.Entirely synthetic antimicrobials.
Are active primarily against gram –ve bacteria.Are active primarily against gram –ve bacteria.
Nalidixic acid- low potency, modest blood andNalidixic acid- low potency, modest blood and
tissue levels, limited spectrum, high resistancetissue levels, limited spectrum, high resistance
Fluoroquinolones –(1 or more flourineFluoroquinolones –(1 or more flourine
substituition ) high potency, expanded spectrum,substituition ) high potency, expanded spectrum,
better tissue penetrance, slow resistance. Theybetter tissue penetrance, slow resistance. They
inhibit the enzyme bacterial DNA gyrase.inhibit the enzyme bacterial DNA gyrase.

CIPROFLOXACINCIPROFLOXACIN
First generation FQ active against a broad rangeFirst generation FQ active against a broad range
of bacteria especially gram –ve aerobic bacilli.of bacteria especially gram –ve aerobic bacilli.
Highly susceptibleHighly susceptible ::
– E coli, shigella,E coli, shigella, NN meningitis, K pneumoniae, Proteus,meningitis, K pneumoniae, Proteus,
H influenza,H influenza, EnterobacterEnterobacter, V. cholerae, S. typhi,, V. cholerae, S. typhi,
NN gonorrhoea.gonorrhoea.
Moderately susceptibleModerately susceptible ::
– Staph aureus, brucella, M. tuberculosisStaph aureus, brucella, M. tuberculosis

Microbiological features :Rapid bactericidalMicrobiological features :Rapid bactericidal
activity and high potency.activity and high potency.
Relatively long post antibiotic effect onRelatively long post antibiotic effect on
enterobacteria, pseudomonas and staph.enterobacteria, pseudomonas and staph.
Low frequency of mutational resistance.Low frequency of mutational resistance.
protective intestinal streptococci and anaerobesprotective intestinal streptococci and anaerobes
are spared.are spared.
Active against manyActive against many ββ lactam and aminolactam and amino
glycoside resistant bacteria.glycoside resistant bacteria.
Less active at acidic pH.Less active at acidic pH.

Adverse effectAdverse effect
GIT – Nausea, vomiting, bad taste, anorexia, diarrhoeaGIT – Nausea, vomiting, bad taste, anorexia, diarrhoea
is infrequent.is infrequent.
CNS- Dizziness, headache, restlessness, anxiety,CNS- Dizziness, headache, restlessness, anxiety,
insomnia and seizures are rare.insomnia and seizures are rare.
Skin/hypersensitivity – rashes, pruritis, urticaria.Skin/hypersensitivity – rashes, pruritis, urticaria.
Tendonitis and tendon ruptureTendonitis and tendon rupture
CIFRAN, CIPLOX, CIPROBID, CIPROLETCIFRAN, CIPLOX, CIPROBID, CIPROLET
Dose :Dose :
– 250, 500,750 mg tab, 200mg/100 ml IV infusion, 3mg/ml eye250, 500,750 mg tab, 200mg/100 ml IV infusion, 3mg/ml eye
drops.drops.

NORFLOXACINNORFLOXACIN
It is less potent than ciproIt is less potent than cipro
It attains lower concentration in tissues.It attains lower concentration in tissues.
It is metabolized as well as excretedIt is metabolized as well as excreted
unchanged in urine.unchanged in urine.
USESUSES
– UTI and Genital infections.UTI and Genital infections.
– Bacterial diarrhea.Bacterial diarrhea.
NORBACTIN, NORFLOX, UROFLOXNORBACTIN, NORFLOX, UROFLOX
Dose :Dose :
– 200, 400, 800 mg tab, 3mg/ml eyedrops200, 400, 800 mg tab, 3mg/ml eyedrops

OFLOXACINOFLOXACIN
Intermediate between Cipro and Norfloxacin inIntermediate between Cipro and Norfloxacin in
activity against Gr-ve bacteriaactivity against Gr-ve bacteria
More potent for Gr +ve organisms andMore potent for Gr +ve organisms and
anaerobesanaerobes
Good activity against chlamydia, alternative drugGood activity against chlamydia, alternative drug
for nonspecific urethritis and atypicalfor nonspecific urethritis and atypical
pneumonia.pneumonia.
Inhibits M tuberculosis; active against M. leprae.Inhibits M tuberculosis; active against M. leprae.
Used in multidrug regimensUsed in multidrug regimens
Dose- 100,200mg tabDose- 100,200mg tab

TETRACYCLINESTETRACYCLINES

TETRACYCLINESTETRACYCLINES
Have a nucleus of four cyclic rings.Have a nucleus of four cyclic rings.
Obtained from soil actinomycetes.Obtained from soil actinomycetes.
First to be introduced – chlortetracycline(1948)First to be introduced – chlortetracycline(1948)
Then oxytetracycline followed.Then oxytetracycline followed.
Tetracyclines are bacteriostatic.(inhibit proteinTetracyclines are bacteriostatic.(inhibit protein
synthesis by binding to 30s ribosomes)synthesis by binding to 30s ribosomes)
Broad spectrum antibioticsBroad spectrum antibiotics

Antimicrobial activityAntimicrobial activity
Gram +ve and –ve cocci are sensitiveGram +ve and –ve cocci are sensitive
Gram +ve bacilli are inhibitedGram +ve bacilli are inhibited
Entero bacteria are highly resistantEntero bacteria are highly resistant
Spirochetes are quite sensitiveSpirochetes are quite sensitive
All rickettsiae and Chlamydia are highlyAll rickettsiae and Chlamydia are highly
sensitivesensitive
Mechanism of action:Mechanism of action:
– Inhibit protein synthesis by binding to 30sInhibit protein synthesis by binding to 30s
ribosomesribosomes

Absorption and excretion:Absorption and excretion:
Tetracyclines have chelating property –Tetracyclines have chelating property –
form insoluble complexes with calciumform insoluble complexes with calcium
and other metals.and other metals.
Milk, iron preparations, and antacids-Milk, iron preparations, and antacids-
reduce their absorption.reduce their absorption.
Doxycycline and minocycline – completelyDoxycycline and minocycline – completely
absorbed, irrespective of food.absorbed, irrespective of food.
They are concentrated in liver, spleen,They are concentrated in liver, spleen,
bone and teeth.bone and teeth.
Excreted by urineExcreted by urine

Adverse effects :Adverse effects :
GIT- epigastric burning, nausea, vomiting,GIT- epigastric burning, nausea, vomiting,
diarrheadiarrhea
Liver damageLiver damage
Renal failureRenal failure
Effects on teeth & bones- Ca tetracycline chelateEffects on teeth & bones- Ca tetracycline chelate
Mid pregnancy-5months deciduous teeth-Mid pregnancy-5months deciduous teeth-
brown, ill formed; 3months-6yrs- permanentbrown, ill formed; 3months-6yrs- permanent
anterior teeth and molars; late pregnancy oranterior teeth and molars; late pregnancy or
childhood- suppression of bone growth.childhood- suppression of bone growth.
Hypersensitivity ReactionsHypersensitivity Reactions
Super infection; Anti-anabolic effectSuper infection; Anti-anabolic effect

DOSEDOSE
Tetracycline – 250-500mg tds in adultsTetracycline – 250-500mg tds in adults
Children over 8yrs -25 to 50mg /kg daily in 2 to 4Children over 8yrs -25 to 50mg /kg daily in 2 to 4
divided dosedivided dose
Doxycycline – 200mg initially, 100-200mg od.Doxycycline – 200mg initially, 100-200mg od.
Ledermycin 150,300mg cap/tabLedermycin 150,300mg cap/tab
RAMYCIN,RESTECLIN-250,500mgcap,50mg/mlRAMYCIN,RESTECLIN-250,500mgcap,50mg/ml
in10ml vial inj DOXT, NOVADOX, TETRADOX-in10ml vial inj DOXT, NOVADOX, TETRADOX-
100mg cap.100mg cap.
Cyanomycin 50,100 mg capCyanomycin 50,100 mg cap

PrecautionPrecaution
Not to be used in pregnancy, lactation andNot to be used in pregnancy, lactation and
in childrenin children
Avoided in patients on diureticsAvoided in patients on diuretics
Used cautiously in renal and hepaticUsed cautiously in renal and hepatic
insufficiencyinsufficiency
Beyond expiry date should not be usedBeyond expiry date should not be used
Do not mix injectable Tc with Pn-Do not mix injectable Tc with Pn-
inactivation occursinactivation occurs

MACROLIDESMACROLIDES

MACROLIDESMACROLIDES
Antibiotics having macrocyclic lactone ring-Antibiotics having macrocyclic lactone ring-
ERYTHROMYCIN-ERYTHROMYCIN-
Isolated from Streptomyces erythreus (1952)Isolated from Streptomyces erythreus (1952)
Alternative to penicillinAlternative to penicillin
Water solubility is limited.solution remains stableWater solubility is limited.solution remains stable
only when kept cold.only when kept cold.
Acts by inhibiting protein synthesis.Acts by inhibiting protein synthesis.
Combines with 50s ribosomes and intereferesCombines with 50s ribosomes and intereferes
with translocationwith translocation

Antibacterial activityAntibacterial activity
Narrow spectrum antibioticNarrow spectrum antibiotic
against penicillin resistant staphylococci.against penicillin resistant staphylococci.
Active against gram +veActive against gram +ve
Pharmacokinetics :Pharmacokinetics :
– Erythromycin base - acid labileErythromycin base - acid labile
– To protect it from gastric acid -Given with entericTo protect it from gastric acid -Given with enteric
coated - incomplete absorptioncoated - incomplete absorption
– Its acid stable esters are better absorbedIts acid stable esters are better absorbed
– Widely distributed in bodyWidely distributed in body
– Excreted through bileExcreted through bile

Dose :Dose :
Adults 250 - 500mg 6hrlyAdults 250 - 500mg 6hrly
Children 30 – 60mg/kg/dayChildren 30 – 60mg/kg/day
Erythromycin base - ERYSAFE 250 mgErythromycin base - ERYSAFE 250 mg
tabtab
Erythromycin stearate -ERYTHROCIN –Erythromycin stearate -ERYTHROCIN –
250,500mg tab250,500mg tab

GIT – epigastric painGIT – epigastric pain
On high doses – hearing impairmentOn high doses – hearing impairment
Hypersensitivity reactions – rareHypersensitivity reactions – rare
UsesUses ::
– Substitute for penicillin, pencillin resistant infectionsSubstitute for penicillin, pencillin resistant infections
– Oral adm, safe and effectiveOral adm, safe and effective
– Perio/periapical/NUG/extractionPerio/periapical/NUG/extraction
– Prophylactic useProphylactic use

ROXITHROMYCINROXITHROMYCIN
Semi synthetic - long acting, acid stableSemi synthetic - long acting, acid stable
macrolidemacrolide
Antibacterial spectrum similar toAntibacterial spectrum similar to
erythromycinerythromycin
DoseDose --
– 150-300mg BD 30min before food150-300mg BD 30min before food
– Children - 2.5-5mg/kg BDChildren - 2.5-5mg/kg BD
– ROXID, ROXIBID 150,300mg tabROXID, ROXIBID 150,300mg tab
– 50mg kid tab,150 mg tab50mg kid tab,150 mg tab

CLINDAMYCINCLINDAMYCIN
It is lincosamide antibiotic having similar actionIt is lincosamide antibiotic having similar action
(macrolide 50s)(macrolide 50s)
Bacteriostatic – low conc;Bacteriocidal – highBacteriostatic – low conc;Bacteriocidal – high
concconc
Most active against gram+ve cocci,Most active against gram+ve cocci,
C.diphtheriae, ActinomycesC.diphtheriae, Actinomyces
Highly active against – anaerobes (B fragilis)Highly active against – anaerobes (B fragilis)
Pharmacokinetics :Pharmacokinetics :
– Oral absorption – goodOral absorption – good
– Distribution – skeletal and soft tissuesDistribution – skeletal and soft tissues
– Excreted in urineExcreted in urine

– Rashes ,UrticariaRashes ,Urticaria
– Abdominal painAbdominal pain
– Superinfection -Enterocolitis &DiarrhoeaSuperinfection -Enterocolitis &Diarrhoea
UsesUses ::
– Anaerobic and mixed infections- alternative to Pn &Anaerobic and mixed infections- alternative to Pn &
macromacro
– Abscess and bone infections-staphy and bacteroidsAbscess and bone infections-staphy and bacteroids
– Infective endocarditisInfective endocarditis
DoseDose ::
– 150-300 mg QID oral ; 200-600mg I.v. 8 hourly150-300 mg QID oral ; 200-600mg I.v. 8 hourly
– DALCAP, CLINCIN, DALCIN, 150, 300 mg cap,DALCAP, CLINCIN, DALCIN, 150, 300 mg cap,
300mg/2ml and 600 mg/4ml inj300mg/2ml and 600 mg/4ml inj

METRANIDAZOLEMETRANIDAZOLE

Anti protozoal/anti amoebic drugsAnti protozoal/anti amoebic drugs
Used in infections caused by protozoa EntamoebaUsed in infections caused by protozoa Entamoeba
histolyticahistolytica
Metranidazole(Flagyl) is considered a bactericidal drugMetranidazole(Flagyl) is considered a bactericidal drug
becos of its fast killing timebecos of its fast killing time
It attacks bacteria’s DNA and works against obligateIt attacks bacteria’s DNA and works against obligate
anaerobesanaerobes
Used in combination with another antibiotic usuallyUsed in combination with another antibiotic usually
amoxicillin, to combat stomach ulcer causingamoxicillin, to combat stomach ulcer causing
Helicobacter pylori.Helicobacter pylori.
Used in periodontal infections to destroy the bacteria thatUsed in periodontal infections to destroy the bacteria that
might infect the root canalmight infect the root canal
Half life is 8-10 hoursHalf life is 8-10 hours
Side effects include an unpleasant metallic taste andSide effects include an unpleasant metallic taste and
brown discolaration of urinebrown discolaration of urine
FLAGYL,METROGYL-200,400mg tabFLAGYL,METROGYL-200,400mg tabwww.indiandentalacademy.comwww.indiandentalacademy.com

ANTIFUNGAL AGENTSANTIFUNGAL AGENTS

Antifungal agentsAntifungal agents
Amphotericin BAmphotericin B
– obtained from - Streptomyces nodususobtained from - Streptomyces nodusus
– Has a Macrocyclic ringHas a Macrocyclic ring
– BBinds to ergosterolinds to ergosterol present in the fungal cellpresent in the fungal cell
membranemembrane and generates poresand generates pores
– Used in serious systemic fungal infectionsUsed in serious systemic fungal infections

Antifungal activity : fungicidal at high conc-staticAntifungal activity : fungicidal at high conc-static
at low conc.at low conc.
Active against-Active against-
– candida albicans, histoplasma, cryptococcuscandida albicans, histoplasma, cryptococcus
neoformans, aspergillusneoformans, aspergillus
Not absorbed orallyNot absorbed orally
Dose :Dose :
– Administered iv as suspension DOCAdministered iv as suspension DOC
– Orally 50-100mg QIDOrally 50-100mg QID
– MYCOL 50mg vialMYCOL 50mg vial
Adverse effects-Adverse effects-
– acute reactions, long term toxicityacute reactions, long term toxicity
Uses : topically – oral,vaginal and cutaneousUses : topically – oral,vaginal and cutaneous
candidiasis.candidiasis.

NYSTATINNYSTATIN
A polyene derived fromA polyene derived from StreptomycesStreptomyces
nourseinoursei
Binds to sterols of fungal cell membraneBinds to sterols of fungal cell membrane
Because of high systemic toxicity used asBecause of high systemic toxicity used as
Topical antifungal agentTopical antifungal agent..
22ndnd
choice to clotrimazolechoice to clotrimazole
1 lac units-4 times a day, 10-14 days1 lac units-4 times a day, 10-14 days
Mycostatin 5 lac U tabMycostatin 5 lac U tab

CLOTRIMAZOLECLOTRIMAZOLE
– Effective in the topical treatment- Esp. athletes foot,Effective in the topical treatment- Esp. athletes foot,
otomycosis and oral, cutaneous candidiasis.otomycosis and oral, cutaneous candidiasis.
well tolerated although Local irritation andwell tolerated although Local irritation and
burningburning
No systemic toxicity is seen after topical use.No systemic toxicity is seen after topical use.
Dose :oropharyngeal candidiasis- 10mg trocheDose :oropharyngeal candidiasis- 10mg troche
-3 to 4 times day.-3 to 4 times day.
SURFAZ, CLOTRIN, CLODERM, 1% lotion,SURFAZ, CLOTRIN, CLODERM, 1% lotion,
cream, powder 100mg tab.cream, powder 100mg tab.
Candid 1% cream, gel, powder.Candid 1% cream, gel, powder.

KETACONAZOLEKETACONAZOLE
– First oral effective broad spectrum antifungal drug.First oral effective broad spectrum antifungal drug.
– The oral absorption of KTZ is facilitated by gastricThe oral absorption of KTZ is facilitated by gastric
acidityacidity
– Hepatic metabolism is extensive metabolites areHepatic metabolism is extensive metabolites are
excreted in urine.excreted in urine.
– The usual dose is 200 mg OD or BDThe usual dose is 200 mg OD or BD
– FUNAZOLE, KETOVATE, FUNGICIDE, 200mg tab,FUNAZOLE, KETOVATE, FUNGICIDE, 200mg tab,
2% oint, cream, shampoo.2% oint, cream, shampoo.
– Nausea and vomiting – loss of appetite, headache,Nausea and vomiting – loss of appetite, headache,
paresthesia, rashes, hair loss.paresthesia, rashes, hair loss.

ANTIVIRAL DRUGSANTIVIRAL DRUGS

ANTI-VIRAL DRUGS.ANTI-VIRAL DRUGS.
AcyclovirAcyclovir
– IndicationsIndications:: Herpes simplex virus (HSV) 1 and 2 infections;Herpes simplex virus (HSV) 1 and 2 infections;
severe genital HSV infections; HSV encephalitis; shingles andsevere genital HSV infections; HSV encephalitis; shingles and
chickenpox; ointment for genital herpes infections; cream forchickenpox; ointment for genital herpes infections; cream for
cold sorescold sores
– Actions:Actions: Inhibits viral DNA replicationInhibits viral DNA replication
– 200mg tab, 5% skin cream200mg tab, 5% skin cream
RimantadineRimantadine
– Indications:Indications: Prophylaxis and treatment of illness caused byProphylaxis and treatment of illness caused by
influenza A virus in adults; prophylaxis against influenza A virusinfluenza A virus in adults; prophylaxis against influenza A virus
in childrenin children
– Actions:Actions: Inhibits viral replication, possibly by preventing theInhibits viral replication, possibly by preventing the
uncoating of the virusuncoating of the virus
– 100mg tab BD100mg tab BD

ANTIBIOTIC PROPHYLAXIS FORANTIBIOTIC PROPHYLAXIS FOR
HEART AND ARTIFICIAL JOINTHEART AND ARTIFICIAL JOINT
PATIENTSPATIENTS

Antibiotics are used for two mainAntibiotics are used for two main
reasons:reasons:
1.1. To treat infectionsTo treat infections
2.2. To prevent infectionsTo prevent infections
Antibiotic prophylaxis is given in patientsAntibiotic prophylaxis is given in patients
who are immunocompromised, patientswho are immunocompromised, patients
with heart ailments and patients with hipwith heart ailments and patients with hip
and joint prosthesisand joint prosthesis
Viridens streptococci are the causativeViridens streptococci are the causative
organisms for seeding heart andorganisms for seeding heart and
implanted joints causing morbidity andimplanted joints causing morbidity and
deathdeath

These s.viridens form colonies on heartThese s.viridens form colonies on heart
valves trapping blood cells and fibrin andvalves trapping blood cells and fibrin and
thereby reducing heart efficiency bythereby reducing heart efficiency by
hindering closure of the valveshindering closure of the valves
These sticky vegetations break off andThese sticky vegetations break off and
lodge in small vessels at distant siteslodge in small vessels at distant sites
causing ischemiacausing ischemia
The goal of antibiotic prophylaxis is toThe goal of antibiotic prophylaxis is to
prevent clinical infections by helpingprevent clinical infections by helping
destroy small number of bacteria presentdestroy small number of bacteria present
before or introduced during treatment.before or introduced during treatment.

Oral procedures requiring prophylaxisOral procedures requiring prophylaxis
Requiring antibioticRequiring antibiotic
prophylaxisprophylaxis
Not requiring prophylaxisNot requiring prophylaxis
ExtractionsExtractions
Periodontal proceduresPeriodontal procedures
Implant placementImplant placement
Tooth reimplantationTooth reimplantation
Placement of orthodonticPlacement of orthodontic
bandsbands
Endodontic instrumentationEndodontic instrumentation
(beyond root apex)(beyond root apex)
Periapical surgeryPeriapical surgery
Intraligamentary injectionIntraligamentary injection
Prophylactic cleaning andProphylactic cleaning and
procedures in which significantprocedures in which significant
bleeding is anticipatedbleeding is anticipated
Operative and prosthodonticOperative and prosthodontic
procedures with or without retractionprocedures with or without retraction
cordcord
LA injectionLA injection
Intracanal endodontic proceduresIntracanal endodontic procedures
Placement of removablePlacement of removable
appliancesappliances
Impression takingImpression taking
Exfoliation of primary toothExfoliation of primary tooth
Oral radiographyOral radiography
FluorideFluoride
Post operative suture removalPost operative suture removal

Standard generalStandard general
AmoxicillinAmoxicillin Adults – 2gAdults – 2g
Children -50mg/kgChildren -50mg/kg
1hr before procedure.1hr before procedure.
Pts unable to takePts unable to take
oral medicationsoral medications
AmpicillinAmpicillin Adults – 2gAdults – 2g
Children -50mg/kgChildren -50mg/kg
IM/IV 30mins beforeIM/IV 30mins before
procedureprocedure
Penicillin allergic ptsPenicillin allergic pts ClindamycinClindamycin
Cephalexin/cefadrCephalexin/cefadr
oxiloxil
Azithromycin/Azithromycin/
clindamycinclindamycin
Adults -600mg;child-Adults -600mg;child-
20mg/kg.20mg/kg.
Adults -2g; child-50mg/kgAdults -2g; child-50mg/kg
Adults-500mg; child-Adults-500mg; child-
15mg/kg.15mg/kg.
1hr before the procedure1hr before the procedure
Pts unable to takePts unable to take
oral medicationsoral medications
ClindamycinClindamycin
cefazolincefazolin
Adults-600mg; child-Adults-600mg; child-
20mg/kg.IV20mg/kg.IV
Adults-1g ; child- 25mg/kgAdults-1g ; child- 25mg/kg
IM/IV.IM/IV.
30mins before procedure.30mins before procedure.

Additional guidelines for antibioticAdditional guidelines for antibiotic
In the case of delayed healing or of a procedure thatIn the case of delayed healing or of a procedure that
involves infected tissues, additional doses of antibioticsinvolves infected tissues, additional doses of antibiotics
may be needed, even though the bacteremia may lastsmay be needed, even though the bacteremia may lasts
for no longer than 15mins after the procedure.for no longer than 15mins after the procedure.
Amoxicillin is the preferred oral antibiotic.Amoxicillin is the preferred oral antibiotic.
If the pt is taking amoxicillin on a long term basis forIf the pt is taking amoxicillin on a long term basis for
some reason, a different class of antibiotic should besome reason, a different class of antibiotic should be
used.used.
If a high risk pt (prosthetic valve) has maintained a highIf a high risk pt (prosthetic valve) has maintained a high
level of oral health, oral antibiotic prophylaxis may belevel of oral health, oral antibiotic prophylaxis may be
used for simple dental procedures rather than parentalused for simple dental procedures rather than parental
regimen.regimen.

ANALGESICSANALGESICS
USED IN ENDODONTICSUSED IN ENDODONTICS

Introduction :Introduction :
Pain is the number one reason people seekPain is the number one reason people seek
health care & has been deemed’’ the fifthhealth care & has been deemed’’ the fifth
vital sign.”vital sign.”
The study of pain has in recent yearsThe study of pain has in recent years
diverged into many different fields fromdiverged into many different fields from
pharmacology to psychology &pharmacology to psychology &
neurobiology.neurobiology.

Definition of painDefinition of pain::
an unpleasant sensory or emotionalan unpleasant sensory or emotional
experience associated with actual or potentialexperience associated with actual or potential
tissue damage or described in terms of suchtissue damage or described in terms of such
damagedamage
a disagreeable sensation produced by the action ofa disagreeable sensation produced by the action of
stimuli of harmful naturestimuli of harmful nature macbryde;1952macbryde;1952
An unpleasant sensation occuring in varyingAn unpleasant sensation occuring in varying
degrees of severity as a consequence of injurydegrees of severity as a consequence of injury
,disease or emotional disorder,disease or emotional disorder..
Medical thesaurusMedical thesaurus

Properties of painProperties of pain
1) Threshold & intensity1) Threshold & intensity
If intensity is lower than the threshold - pain isIf intensity is lower than the threshold - pain is
not feltnot felt
Weber –Fechners law:Weber –Fechners law:
100 fold increase in intensity =3 fold100 fold increase in intensity =3 fold
increaseincrease
in painin pain
2)Adaptation2)Adaptation
Pain receptors show no adaptation,painPain receptors show no adaptation,pain
continues ascontinues as
long as receptors are stimulatedlong as receptors are stimulated

3) Localisation of pain3) Localisation of pain
Superficial pain is comparatively betterSuperficial pain is comparatively better
localised than deep pain. Visceral pain islocalised than deep pain. Visceral pain is
usually referredusually referred
4)Emotional accompaniment4)Emotional accompaniment::
associated emotions are unpleasantassociated emotions are unpleasant
5) Influence of the rate of damage on the5) Influence of the rate of damage on the
intensity of pain :intensity of pain :

If the rate of injury is high intensity of pain is also highIf the rate of injury is high intensity of pain is also high
A very slowly growing tissue damaging agent eg:A very slowly growing tissue damaging agent eg:
cancer at an early stage may not produce pain at all.cancer at an early stage may not produce pain at all.
6) Double pain:6) Double pain:
Due to the initial action on a-delta fibres;followed by c-Due to the initial action on a-delta fibres;followed by c-
fibres.fast pain is better localised than slow pain.fibres.fast pain is better localised than slow pain.

Biochemical basis of painBiochemical basis of pain::
neurotransmittersneurotransmitters
neuromodulatorsneuromodulators
Neurotransmitters:Neurotransmitters:
are substances that are synthesizedare substances that are synthesized
& stored in the neuron for release during& stored in the neuron for release during
neural activity.neural activity.
NeuromodulatorsNeuromodulators
are substances that modify theare substances that modify the
release of neurotransmitters from pre-release of neurotransmitters from pre-
synaptic terminalssynaptic terminals

Neurotransmitters are classified intoNeurotransmitters are classified into::
1) Excitatory agents:1) Excitatory agents:
Ach , norepinephrine,Ach , norepinephrine, glutamate,glutamate,
substancePsubstanceP,,
histaminehistamine
2) Inhibitory agents:2) Inhibitory agents:
serotonineserotonine, GABA, endorphins, glycine,, GABA, endorphins, glycine,
somatostatin, dopamine.somatostatin, dopamine.
3) Inflammatory agents:3) Inflammatory agents:
prostaglandins, bradykininprostaglandins, bradykinin

Glutamate:Glutamate:
Amino acid secreted by pre-synaptic terminalsAmino acid secreted by pre-synaptic terminals
Found in the spinal cord dorsal horn & isFound in the spinal cord dorsal horn & is
associated with noxious input.associated with noxious input.
Substance PSubstance P ::
Polypeptide,composed of 11 amino acidsPolypeptide,composed of 11 amino acids
Released at the terminals of primaryReleased at the terminals of primary
nociceptive neuronsnociceptive neurons
Also released from spinal cord byAlso released from spinal cord by
stimulation with A-delta & C-fibresstimulation with A-delta & C-fibres

Serotonin:Serotonin:
Secreted in the brain stem & project down to theSecreted in the brain stem & project down to the
spinal cordspinal cord
Imp. Inhibitory neurotransmitter in the C.N.SImp. Inhibitory neurotransmitter in the C.N.S
Central serotoninis thought to potentiateCentral serotoninis thought to potentiate
endorphin analgesiaendorphin analgesia
Prostaglandins:Prostaglandins:
PGE2 metabolised from arachidionic acidPGE2 metabolised from arachidionic acid
Sensitize nerve endings to nociceptive stimuliSensitize nerve endings to nociceptive stimuli
BradykininBradykinin::
Released as part of the inflammatory reactionReleased as part of the inflammatory reaction
Acts as an allogenic agent that excites all kinds ofActs as an allogenic agent that excites all kinds of
receptorsreceptors
Also sensitizes some high threshold receptorsAlso sensitizes some high threshold receptors
Requires the presence of PG’s to act.Requires the presence of PG’s to act.

Classification of painClassification of pain
Primary –injury ,neuropathic painPrimary –injury ,neuropathic pain
Secondary-referred painSecondary-referred pain
AcuteAcute
ChronicChronic
Primary painPrimary pain::
inflammatoryinflammatory : following injury pain sets in & persists until: following injury pain sets in & persists until
healinghealing ; characteristically produces hyperalgesia & allodynia; characteristically produces hyperalgesia & allodynia
Hyperalgesia :Hyperalgesia : an increased response to a stimulus that isan increased response to a stimulus that is
normally painfulnormally painful
AllodyniaAllodynia : pain due to a stimulus that does not normally provoke: pain due to a stimulus that does not normally provoke
pain.pain.
Referred painReferred pain::
pain in a part of body that is fairly remote from thepain in a part of body that is fairly remote from the
site of originsite of origin

ACUTE PAINACUTE PAIN
Sharp,fast ,prickingSharp,fast ,pricking
typetype
Occurs in 0.1 secs ofOccurs in 0.1 secs of
stimulusstimulus
Carried by large caliberCarried by large caliber
myelinated A-deltamyelinated A-delta
fibersfibers
Speed of travel-6-30Speed of travel-6-30
m/secm/sec
CHRONIC PAINCHRONIC PAIN
Slow,burning,achingSlow,burning,aching
gradually increasesgradually increases
after 1 sec of stimulusafter 1 sec of stimulus
small calibersmall caliber
unmyelinated C-fibersunmyelinated C-fibers
Speed of travel 0.5-Speed of travel 0.5-
2m/sec2m/sec

 The sensory input from the face and the mouthThe sensory input from the face and the mouth
is carried by way of the fifth cranial nerve ;is carried by way of the fifth cranial nerve ;THETHE
TRIGEMINAL NERVE.TRIGEMINAL NERVE.
 The cell bodies of the trigeminal afferentThe cell bodies of the trigeminal afferent
neurons are located in theneurons are located in the Large GasserianLarge Gasserian
GanglionGanglion
 Impulses carried by the trigeminal nerve enterImpulses carried by the trigeminal nerve enter
directly into the brain stem in the region of thedirectly into the brain stem in the region of the
PonsPons to synapse in theto synapse in the trigeminal spinal tracttrigeminal spinal tract
nucleus.nucleus.
 This region is very similar to the dorsal horn ofThis region is very similar to the dorsal horn of
the spinal cord and is sometimes referred to asthe spinal cord and is sometimes referred to as
the medullary dorsal hornthe medullary dorsal horn

The brain stem- trigeminal nucleusThe brain stem- trigeminal nucleus
complex consists of the main sensorycomplex consists of the main sensory
trigeminal nucleus which is rostrallytrigeminal nucleus which is rostrally
located and receives periodontal andlocated and receives periodontal and
some pulpal afferents; and the spinal tractsome pulpal afferents; and the spinal tract
of the trigeminal nucleus which is moreof the trigeminal nucleus which is more
caudally locatedcaudally located

Motor nucleusMotor nucleus
Another component of the trigeminal brainAnother component of the trigeminal brain
stem complex is thestem complex is the motor nucleus of themotor nucleus of the
Vth nerve.Vth nerve.
This area is involved interpretation ofThis area is involved interpretation of
impulses that require motor responses orimpulses that require motor responses or
reflexes.reflexes.

The endogenous pain inhibiting mechanismThe endogenous pain inhibiting mechanism
The degree to which a person reacts to painThe degree to which a person reacts to pain
varies tremendously. This results partly from avaries tremendously. This results partly from a
capability of the brain itself to suppress input ofcapability of the brain itself to suppress input of
pain signals to the nervous system by activatingpain signals to the nervous system by activating
a pain control system, called ana pain control system, called an analgesiaanalgesia
system.system.
Several transmitter substances are involved inSeveral transmitter substances are involved in
the analgesia system; especially involved arethe analgesia system; especially involved are
EnkephalinEnkephalin oror Serotonin,Serotonin, secreted by manysecreted by many
nerve fibers (enkephalinergic or serotogenicnerve fibers (enkephalinergic or serotogenic
neurons) derived from the Periventricular nucleineurons) derived from the Periventricular nuclei
and from the Periaqueductal gray areaand from the Periaqueductal gray area

These neurons synapse with the A and CThese neurons synapse with the A and C
fiber terminals at the substantiafiber terminals at the substantia
gelatinosa rolandi (SGR )which bring paingelatinosa rolandi (SGR )which bring pain
from the periphery in the posterior horn offrom the periphery in the posterior horn of
the spinal cord.the spinal cord.
These fibers when stimulated releaseThese fibers when stimulated release
enkephalin or serotonin an endogenousenkephalin or serotonin an endogenous
opiod peptide which inhibits the pain.opiod peptide which inhibits the pain.

The pain phenomenon:The pain phenomenon:
Pain is always subjective due toPain is always subjective due to
modulation and cross over in the CNSmodulation and cross over in the CNS
The process begins in the periphery whereThe process begins in the periphery where
specialized nerve fibers receive a painfulspecialized nerve fibers receive a painful
stimulus.stimulus.
This information passes through theThis information passes through the
Spinal cord to reach the brain and theSpinal cord to reach the brain and the
brain interprets the information as painbrain interprets the information as pain

The spinal tract nucleus STN is dividedThe spinal tract nucleus STN is divided
into three regionsinto three regions
1)1) Subnucleus OralisSubnucleus Oralis
2)2) Subnucleus InterpolarisSubnucleus Interpolaris
3)3) Subnucleus CaudalisSubnucleus Caudalis, which, which
corresponds to the medullary dorsal horncorresponds to the medullary dorsal horn
Tooth pulp afferent fibers go to all threeTooth pulp afferent fibers go to all three
subnucleisubnuclei

Second order trigeminal neurons project to the thalamusSecond order trigeminal neurons project to the thalamus
from synaptic junctions with primary afferents in thefrom synaptic junctions with primary afferents in the
subnucleus caudalissubnucleus caudalis
As in the dorsal horn these interneurons represent threeAs in the dorsal horn these interneurons represent three
types oftypes of Transmission CellsTransmission Cells oror T cellsT cells. They are. They are
1)1) Wide dynamic range neurons (WDR)Wide dynamic range neurons (WDR)
2)2) Nociceptive specific neurons (NS)Nociceptive specific neurons (NS)
3)3) Low threshold mechanoreceptive (LTM) afferentsLow threshold mechanoreceptive (LTM) afferents
The WDR and NS neurons dominate in lamina I,II,IVThe WDR and NS neurons dominate in lamina I,II,IV
and comprise the trigeminal nociceptive pathway. Theyand comprise the trigeminal nociceptive pathway. They
all receive input from cutaneous structures and at leastall receive input from cutaneous structures and at least
half of them receive input from deep structures of thehalf of them receive input from deep structures of the
mouth and face.mouth and face.

Detection of Odontogenic painDetection of Odontogenic pain
Odontogenic pain transmission is mediatedOdontogenic pain transmission is mediated
primarily by the peripheral sensoryprimarily by the peripheral sensory
neurons of the trigeminal nerve.Theneurons of the trigeminal nerve.The
peripheral terminals of these nervesperipheral terminals of these nerves
innervate the dental pulp and other oralinnervate the dental pulp and other oral
tissues, whereas the central terminalstissues, whereas the central terminals
release neurotransmitters such asrelease neurotransmitters such as
substance P, which are involved in thesubstance P, which are involved in the
initiation of paininitiation of pain

These trigeminal sensory afferent neurons alongThese trigeminal sensory afferent neurons along
with the sympathetic branches of the superiorwith the sympathetic branches of the superior
cervical ganglion and blood vessels, entercervical ganglion and blood vessels, enter
through the apical foramen of a tooth. together,through the apical foramen of a tooth. together,
these nerves and blood vessels form thethese nerves and blood vessels form the
neurovascular bundle. These nerve fibers are :neurovascular bundle. These nerve fibers are :
Myelinated UnmyelinatedMyelinated Unmyelinated
A fibers ( alpha , beta, gamma & delta)
C fibers
0.5-1μ dia, 0.5-2 m/s vel6-13μ dia , 40-70 m/s vel
1-5μ dia, 5-15 m/s vel
β
δ

Pulpal sensory nerve activity:
Mainly there are three types of fibers are found in the pulp:
Alfa and Beta Fibers
* Fast conducting
* Role not known
A-DELTA
FIBERS
•Fast conducting
•Low threshold
•Myelinated
A BETA FIBERS
Fastest conducting
Of all intradental fibers
Serve as mechanoreceptors
As trigger for withdrawal reflexes
C-TYPE
FIBERS
Slow
conducting
High threshold
Un myelinated
*** Whenever the pulpal blood flow is increases it has an
excitatory effect
on A-Delta and C-type fibers.
A-Delta C-Fibers
Sharp, piercing and
Lancinating type of
Pain
Dull, boring, gnawing and
Excruciating pain.

A Delta fibersA Delta fibers
Most common in dental pulpMost common in dental pulp
They are referred to as NOCICEPTIVE FIBERSThey are referred to as NOCICEPTIVE FIBERS
Once beneath the odontoblastic layer they looseOnce beneath the odontoblastic layer they loose
their myelin sheath anastomose and form thetheir myelin sheath anastomose and form the
PLEXUS OF RASHKOWPLEXUS OF RASHKOW
The free nerve endings extend 200μ m into theThe free nerve endings extend 200μ m into the
dentinal tubules ( pulpo dentinal complex)dentinal tubules ( pulpo dentinal complex)
Produces momentary quick sharp painProduces momentary quick sharp pain

C nerve fibersC nerve fibers
High threshold unmyelinated fibersHigh threshold unmyelinated fibers
Run subjacent to delta fibersRun subjacent to delta fibers
Not directly involved in the pulpodentinal complex andNot directly involved in the pulpodentinal complex and
less easily provokedless easily provoked
Dull poorly localized painDull poorly localized pain
Activate by intense heating or coolingActivate by intense heating or cooling
Once activated the pain can radiate anywhere in theOnce activated the pain can radiate anywhere in the
ipsilateral face and jawsipsilateral face and jaws
Stimulated C fibers release inflammatory modulatorsStimulated C fibers release inflammatory modulators
such as substance P and calcitonin gene related peptidesuch as substance P and calcitonin gene related peptide
(CGRP)(CGRP)
More resistant to compromised blood flow than A deltaMore resistant to compromised blood flow than A delta
fibersfibers

ProcessingProcessing
The input from the teeth and periradicular regionThe input from the teeth and periradicular region
is transmitted by the maxillary and mandibularis transmitted by the maxillary and mandibular
branches of trigeminal nerve to the CNSbranches of trigeminal nerve to the CNS
The primary afferent neurons enters the brainThe primary afferent neurons enters the brain
stem at the level of the pons.stem at the level of the pons.
The primary neuron synapses with a secondThe primary neuron synapses with a second
order neuron in the sub nucleus caudalis regionorder neuron in the sub nucleus caudalis region
of the trigeminal spinal tract nucleusof the trigeminal spinal tract nucleus
From here the impulse is carried to theFrom here the impulse is carried to the
thalamus.thalamus.
The second order neuron crosses the brain stemThe second order neuron crosses the brain stem
to the opposite side of the brain and ascends toto the opposite side of the brain and ascends to
the higher centersthe higher centers

A delta fibers from the pulp synapse in theA delta fibers from the pulp synapse in the
lamina I area of the subnucleus caudalis and clamina I area of the subnucleus caudalis and c
fibers synapse in the lamina II and III areas .fibers synapse in the lamina II and III areas .
A delta neurons pass to the thalamus directly byA delta neurons pass to the thalamus directly by
the way of the neospinothalamic tract.the way of the neospinothalamic tract.
The pathway ascends to the thalamus directlyThe pathway ascends to the thalamus directly
and is said to carryand is said to carry fast pain.its sharp and easyfast pain.its sharp and easy
to localizeto localize
The second order C fibers neuron carriesThe second order C fibers neuron carries
impulses via the the paleospinothalamic tract.impulses via the the paleospinothalamic tract.

This passes through the reticular formation , where theThis passes through the reticular formation , where the
impulses are influenced by many modulating processesimpulses are influenced by many modulating processes
before they reach the thalamus, since these impulsesbefore they reach the thalamus, since these impulses
take longer to reach the thalamus the pain is calledtake longer to reach the thalamus the pain is called slowslow
pain.( dull aching)pain.( dull aching)
Once the nociceptive input reaches the sensory cortexOnce the nociceptive input reaches the sensory cortex
in the parietal lobe pain recognition occurs.in the parietal lobe pain recognition occurs.
The cortex may rely on memory of previous experienceThe cortex may rely on memory of previous experience
of dental pain to recognize the input as pain.of dental pain to recognize the input as pain.
In addition to the trigeminal path pain is also mediated byIn addition to the trigeminal path pain is also mediated by
sympathetic and some parasympathetic afferent nervesympathetic and some parasympathetic afferent nerve
fibers and 7fibers and 7thth
, 9, 9thth
and 10and 10thth
cranial nerves which supply thecranial nerves which supply the
oral region.oral region.

PerceptionPerception
The final step in the subjective process isThe final step in the subjective process is
perception , this happens when the inputperception , this happens when the input
reaches the cortex.reaches the cortex.
And perception differs from patient to patientAnd perception differs from patient to patient
depending on past experience, emotionaldepending on past experience, emotional
state,cultural factors etc.state,cultural factors etc.
Orofacial pain may produce unreasonableOrofacial pain may produce unreasonable
anxiety in the patient and this is why itsanxiety in the patient and this is why its
important for the clinician to identify the sourceimportant for the clinician to identify the source
of the pain..of the pain..

Management of painManagement of pain
Anaelgesics are drugs which relieve painAnaelgesics are drugs which relieve pain
without loss of consciousness.without loss of consciousness.
They offer symptomatic relief from painThey offer symptomatic relief from pain
without affecting its causewithout affecting its cause
They are of two classesThey are of two classes
1.1. Opoid or morphine type of analgesicsOpoid or morphine type of analgesics
2.2. Non-opiod or aspirin type of analgesicsNon-opiod or aspirin type of analgesics

Opioid analgesics:Opioid analgesics:
1.1. Opium is in use since 4000 BCOpium is in use since 4000 BC
2.2. Opioid is a term used for drugs with morphine likeOpioid is a term used for drugs with morphine like
actionsactions
3.3. Earlier called as Narcotic analgesicsEarlier called as Narcotic analgesics
Classification:Classification:
1.1. Agonists :Agonists :
-natural opium alkaloids,eg morphine,codeine-natural opium alkaloids,eg morphine,codeine
-synthetic opiods,eg. Pethidine, methadone-synthetic opiods,eg. Pethidine, methadone
-semisynthetic opiates-Diacetylmorphine(heroin),-semisynthetic opiates-Diacetylmorphine(heroin),
pholcodeine.Hydrocodone, oxycodone are not av. Inpholcodeine.Hydrocodone, oxycodone are not av. In
indiaindia
2. Antagonists : Naloxone, Naltrexone.2. Antagonists : Naloxone, Naltrexone.
3. Mixed agonist-antagonists : Pentazocine, Nalbuphine,3. Mixed agonist-antagonists : Pentazocine, Nalbuphine,
NalorpineNalorpine

Morphine :Morphine :
Mechanism of action- act on specific opiodMechanism of action- act on specific opiod
receptors.receptors.
- The opiod receptors are- The opiod receptors are
mu, kappa, deltamu, kappa, delta
- Endogenous opiod peptides released in- Endogenous opiod peptides released in
response to pain are enkephalines, theresponse to pain are enkephalines, the
endorphins, and dynorphinsendorphins, and dynorphins

Relieves pain without loss of consciousnessRelieves pain without loss of consciousness
It alters perception and reaction to painIt alters perception and reaction to pain
Raises pain threshold and increases capacity toRaises pain threshold and increases capacity to
tolerate paintolerate pain
Euphoria and sedation add to its analgesicEuphoria and sedation add to its analgesic
effectseffects
Bioavailability- 20-40 %,onset of action is 15-Bioavailability- 20-40 %,onset of action is 15-
20 min, duration of action- 3-5 hr20 min, duration of action- 3-5 hr
Morphine produces adverse effects like nausea,Morphine produces adverse effects like nausea,
vomiting ,dizziness, hypotensionvomiting ,dizziness, hypotension
Morphine is Histamine liberator and this actionMorphine is Histamine liberator and this action
is responsible for allergic effectsis responsible for allergic effects

Dose: 10-20mg IM/SC, 20 mg tabDose: 10-20mg IM/SC, 20 mg tab
available ( ethyl morphine)available ( ethyl morphine)
Acute morphine poisoning may beAcute morphine poisoning may be
accidental, suicidal or homicidalaccidental, suicidal or homicidal
Lethal dose- 250 mg ,coma and deathLethal dose- 250 mg ,coma and death
occur due to res. failure and pulmonaryoccur due to res. failure and pulmonary
oedemaoedema
Gastric lavage with potassiumGastric lavage with potassium
permanganate to remove unabsorbedpermanganate to remove unabsorbed
drugdrug
Specific antidote is naloxone- 0.4 -0.8 mgSpecific antidote is naloxone- 0.4 -0.8 mg
iv repeated every 10-15 minsiv repeated every 10-15 mins

Codeine and pethidine are other opiodCodeine and pethidine are other opiod
analgesics used in 25-30 mg dosagesanalgesics used in 25-30 mg dosages
They are less potent than morphineThey are less potent than morphine
Their duration of action is much shorterTheir duration of action is much shorter
and onset of action is more rapid thanand onset of action is more rapid than
morphinemorphine

Selected opioid combination Analgesic drugsSelected opioid combination Analgesic drugs
are:are:
1.1. Acetaminophen (300mg) and Codeine(30mg)-Acetaminophen (300mg) and Codeine(30mg)-
Tylenol with codeine (trade name)- dose-2 tabsTylenol with codeine (trade name)- dose-2 tabs
q4hq4h
2.2. Acetaminophen(500mg) andAcetaminophen(500mg) and
hydrocodone(5mg)- Vicodin, lortabhydrocodone(5mg)- Vicodin, lortab
dose-1-2 tab q6hdose-1-2 tab q6h
3. Aspirin (325mg) and Codeine(30mg)- 2 tabs3. Aspirin (325mg) and Codeine(30mg)- 2 tabs
q4h (Empirin with codeine no.3)q4h (Empirin with codeine no.3)
4.4. Aspirin (325mg) and oxycodone (5mg)_Aspirin (325mg) and oxycodone (5mg)_
Percodan – 1 tab eachPercodan – 1 tab each

NON-STEROIDAL ANTI-INFLAMMATORYNON-STEROIDAL ANTI-INFLAMMATORY
DRUGS ( NSAIDS )DRUGS ( NSAIDS )
Aspirin type or non opioid analgesicsAspirin type or non opioid analgesics
They do not depress CNS and they act onThey do not depress CNS and they act on
peripheral pain mechanismsperipheral pain mechanisms
They have anti inflammatory , antipyreticThey have anti inflammatory , antipyretic
and analgesic properties without addictionand analgesic properties without addiction
liabilityliability
The active principle ‘salicin’ was isolatedThe active principle ‘salicin’ was isolated
from bark of willow tree and is convertedfrom bark of willow tree and is converted
into glucose and salicylic acid in the bodyinto glucose and salicylic acid in the body

CLASSIFICATIONCLASSIFICATION
1.1. Salicylic acid derivative – Aspirin,Sodium salicylate,Salicylic acid derivative – Aspirin,Sodium salicylate,
2.2. Para amino phenol derivatives- paracetamolPara amino phenol derivatives- paracetamol
3.3. Pyrazolone derivatives- phenyl butazone,Pyrazolone derivatives- phenyl butazone,
AzapropazoneAzapropazone
4.4. Indole acetic acid derivatives- indomethacin,sulindacIndole acetic acid derivatives- indomethacin,sulindac
5.5. Aryl acetic acid derivatives- Diclofenac,Ketoralac,Aryl acetic acid derivatives- Diclofenac,Ketoralac,
TolmetinTolmetin
6.6. Propionic acid derivatives- Ibuprofen, FenoprofenPropionic acid derivatives- Ibuprofen, Fenoprofen
7.7. Anthranilic acid- Flufenamic acid,Mefenamic acidAnthranilic acid- Flufenamic acid,Mefenamic acid
8.8. OxIcams- Piroxicam, TenoxicamOxIcams- Piroxicam, Tenoxicam
9.9. Alkanones- nabumetone,Alkanones- nabumetone,
10.10. Sulfonanilide derivatives- nimuselide, celecoxibSulfonanilide derivatives- nimuselide, celecoxib

Mechanisim of actionMechanisim of action
Arachidonic acid liberated fromArachidonic acid liberated from
membrane phospholipids duringmembrane phospholipids during
inflammation is converted toinflammation is converted to
prostaglandins catalyzed by the enzymeprostaglandins catalyzed by the enzyme
cyclo-oxygenasecyclo-oxygenase
These prostoglandins produceThese prostoglandins produce
hyperalgesia which sensitize nervehyperalgesia which sensitize nerve
endings to pain and other mediators ofendings to pain and other mediators of
inflammation like bradykinin and histamininflammation like bradykinin and histamin
These NSAIDs inhibit the PG synthesis byThese NSAIDs inhibit the PG synthesis by
inhibiting the enzyme cyclo-oxygenaseinhibiting the enzyme cyclo-oxygenase

Cox-2 inhibitors: new analgesic and anti-Cox-2 inhibitors: new analgesic and anti-
inflammatory drugsinflammatory drugs
Although NSAID’s are effective in managementAlthough NSAID’s are effective in management
of pain and inflammation , their use is limited byof pain and inflammation , their use is limited by
several side effects like git bleeding andseveral side effects like git bleeding and
ulceration,impaired renal function and inhibitionulceration,impaired renal function and inhibition
of platelet aggregationof platelet aggregation
This new generation of selectiveThis new generation of selective
cyclooxegenase-2(cox-2) inhibitors holdcyclooxegenase-2(cox-2) inhibitors hold
promise for achieving therapeutic effects ofpromise for achieving therapeutic effects of
traditional NSAID’s without deleterious sidetraditional NSAID’s without deleterious side
effectseffects

Two isoforms of COX enzyme: cox-1 and cox-2Two isoforms of COX enzyme: cox-1 and cox-2
These cox-2 inhibitors selectively act on cox-2These cox-2 inhibitors selectively act on cox-2
and have no effect on cox-1.and have no effect on cox-1.
Celecoxib is the first selective Cox-2 inhibitor toCelecoxib is the first selective Cox-2 inhibitor to
be introduced. It was used in a dose of 200mgbe introduced. It was used in a dose of 200mg
orallyorally
Rofecoxib was introduced later and is reportedRofecoxib was introduced later and is reported
to be more selective for cox-2 than Celecoxib.Itto be more selective for cox-2 than Celecoxib.It
is used in a dose of 50mg once dailyis used in a dose of 50mg once daily
Used in caution in patients with impaired renalUsed in caution in patients with impaired renal
functionfunction

DRUGDRUG DOSAGEDOSAGE PROPERTIESPROPERTIES ADVANTAGESADVANTAGES USESUSES
AspirinAspirin
Salicylic acidSalicylic acid
derivativederivative
AnalgesicAnalgesic
-300--300-
600mg/6-8hrs600mg/6-8hrs
Anti-Anti-
inflammatoryinflammatory
4-6gm/day4-6gm/day
Good analgesic ,Good analgesic ,
anti-pyretic, anti-anti-pyretic, anti-
Gastric irritantGastric irritant
Powerful anti-Powerful anti-
inflammatory andinflammatory and
anti-plateletanti-platelet
activityactivity
Pyrexia,Pyrexia,
headache,backacheadache,backac
he,he,
Rheumatic feverRheumatic fever
AcetaminopheAcetaminophe
n (Tylenol)n (Tylenol)
Para-Para-
aminophenolaminophenol
0.5-1gm(3-60.5-1gm(3-6
times daily)times daily)
Max-4gMax-4g
Good analgesic,Good analgesic,
anti pyretic, pooranti pyretic, poor
anti-inflammatoryanti-inflammatory
Less gastricLess gastric
irritationirritation
As analgesicAs analgesic
Anti pyretic,Anti pyretic,
chronic pulpitis,chronic pulpitis,
peridontalperidontal
abscessabscess
DiclofenacDiclofenac
-Indole-Indole
acetic acidacetic acid
50mg50mg
BD/TDSBD/TDS
Analgesic, anti-Analgesic, anti-
pyretic, anti-pyretic, anti-
Gel for topicalGel for topical
applicationapplication
GoodGood
concentration inconcentration in
synovial fluid,synovial fluid,
adverse effectsadverse effects
mildmild
ChronicChronic
conditions,conditions,
rheumatoid arthritis,rheumatoid arthritis,
osteoarthritis, acuteosteoarthritis, acute
pulpitis, periapicalpulpitis, periapical
abscessabscess
PiroxicamPiroxicam
OxicamOxicam
20mg OD20mg OD Analgesic, anti-Analgesic, anti-
Long actingLong acting
Better toleratedBetter tolerated
Arthritis,Arthritis,
musculoskeletalmusculoskeletal
pain , post-pain , post-
operative painoperative pain

DRUGDRUG DOSEDOSE PROPERTIESPROPERTIES ADVANTAGESADVANTAGES USESUSES
PhenylbutazonePhenylbutazone
PyrazolonePyrazolone
100-200mg,100-200mg,
BDBD
Good anti-Good anti-
inflammatory, poorinflammatory, poor
analgesic,anti-analgesic,anti-
pyretic, waterpyretic, water
retention causesretention causes
oedemaoedema
Powerful antiPowerful anti
Rheumatoid andRheumatoid and
osteoarthritis,osteoarthritis,
gout, ankylosinggout, ankylosing
spondilitisspondilitis
IndomethacinIndomethacin
Indole acetic acidIndole acetic acid
25-50mg, 3-525-50mg, 3-5
times/daytimes/day
Toxicity is highToxicity is high
Potent antiPotent anti
inflammatory andinflammatory and
analgesicanalgesic
Rheumatoid,Rheumatoid,
psoriatic andpsoriatic and
osteoarthritis,osteoarthritis,
gout, ankylosinggout, ankylosing
spondilitis, closurespondilitis, closure
of PDAof PDA
CelecoxibCelecoxib
RofecoxibRofecoxib
Cox-2 inhibitorsCox-2 inhibitors
100-200mg100-200mg
twice dailytwice daily
50mg/day50mg/day
Effective antiEffective anti
inflammatory agentinflammatory agent
Cox2 inhibitorCox2 inhibitor
Less side effectsLess side effects
and lessand less
ulcerogeniculcerogenic
Rheumatoid andRheumatoid and
osteoarthritisosteoarthritis
IbuprofenIbuprofen
Propionic acidPropionic acid
400-800mg400-800mg
TDSTDS
Milder than aspirinMilder than aspirin
Adverse effectsAdverse effects
milder, bettermilder, better
toleratedtolerated
Analgesic, antiAnalgesic, anti
pyretic, soft tissuepyretic, soft tissue
injuries, fractures,injuries, fractures,
chronic pulpitis,chronic pulpitis,
periodontal andperiodontal and
gingival abscessgingival abscess

CorticosteroidsCorticosteroids
Used in cases of post endodontic flareupsUsed in cases of post endodontic flareups
Inflammatory mediators are released into theInflammatory mediators are released into the
tissues causing vascular dilatationtissues causing vascular dilatation
Glucocorticoids are used to reduce the acuteGlucocorticoids are used to reduce the acute
inflammatory response by suppressinginflammatory response by suppressing
vasodilatation, migration of PMN leucocytes, andvasodilatation, migration of PMN leucocytes, and
phagocytosis and by inhibiting the formation ofphagocytosis and by inhibiting the formation of
arachidonic acid from neutrophil andarachidonic acid from neutrophil and
macrophage cell membrane phospholipids thusmacrophage cell membrane phospholipids thus
blocking cyclooxygenase and lipooxygenaseblocking cyclooxygenase and lipooxygenase
pathways and respective synthesis ofpathways and respective synthesis of
prostaglandins and leukotrienesprostaglandins and leukotrienes

Glucocorticoids are secreted by adrenalGlucocorticoids are secreted by adrenal
gland in response to ultradian andgland in response to ultradian and
circadian rhythms and to stresscircadian rhythms and to stress
They are available as systemic as well asThey are available as systemic as well as
topical formstopical forms
Commonly used areCommonly used are
cortisone-20-300 mg/daycortisone-20-300 mg/day
hydrocortisone-20-240mg/dayhydrocortisone-20-240mg/day
prednisone-5-60mg/dayprednisone-5-60mg/day

ANTI ANXIETY DRUGSANTI ANXIETY DRUGS(ANXIOLYTICS)(ANXIOLYTICS)
Anxiety is tension or apprehension whichAnxiety is tension or apprehension which
is a normal response to certain situationsis a normal response to certain situations
in life.in life.
Universal human emotionUniversal human emotion
But when excessive and disproportionateBut when excessive and disproportionate
to the situation it becomes disabling andto the situation it becomes disabling and
needs treatmentneeds treatment

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